Solvation-Mediated Self-Assembly from Crystals to Helices of Protic Acyclic Carbene AuI -Enantiomers with Chirality Amplification.

Constructing chiral supramolecular assembly and exploring the underlying mechanism are of great significance in promoting the development of circularly polarized luminescence (CPL)-active materials. Herein, we report a solvation-mediated self-assembly from single-crystals to helical nanofibers based on the first protic acyclic (methoxy)(amino)carbenes (pAMACs) AuI -enantiomers driven by a synergetic aurophilic interactions and H-bonds. Their aggregation-dependent thermally activated delayed fluorescence properties with high quantum yields (ΦFL ) up to 95 % were proved to be attributed to packing modes of Au⋅⋅⋅Au dimers with π-stacking or one-dimensional extended Au⋅⋅⋅Au chains. Via drop-casting method, supramolecular P- or M-helices were prepared. Detailed studies on the helices demonstrate that formations of extended helical Au⋅⋅⋅Au molecular chains amplify supramolecular chirality, leading to strong CPL with high dissymmetry factor (|glum |=0.030, ΦFL =67 %) and high CPL brightness (BCPL ) of 4.87×10-3 . Our findings bring new insights into the fabrication of helical structures to improve CPL performance by modifying aurophilic interactions.

Nirmatrelvir/ritonavir use in patients with COVID-19 on hemodialysis: a case series.

Patients undergoing hemodialysis (HD) are particularly vulnerable to coronavirus disease 2019 (COVID-19) and are at increased risk of developing severe infection. However, given the exclusion of such patients from clinical trials, there are limited data regarding the effectiveness of the antiviral drug nirmatrelvir/ritonavir (N/R) in patients on HD. We prescribed N/R to 4 patients on HD with COVID-19 after obtaining informed consent. Their clinical symptoms were improved at approximately 3 days after N/R administration. The viral load was reduced after approximately 10 days. The main adverse effects were nausea and vomiting. Rational dosage adjustment obtained good tolerance but did not influence the efficacy. These results suggest that N/R may be a promising agent for patients on HD with COVID-19.

Fluorinated poly(p-triphenyl piperidine) anion exchange membranes with robust dimensional stability for fuel cells.

Anion exchange membrane fuel cells (AEMFCs), which are more economical than proton exchange membrane fuel cells (PEMFCs), stand out in the context of the rapid development of renewable energy. Superacid-catalyzed ether-free aromatic polymers have recently received a lot of attention due to their exceptional performance, but their development has been hampered by the trade-off between the dimensional stability and ionic conductivity of anion exchange membranes (AEMs). Here, we introduced fluoroketones containing different numbers of fluorinated groups (x = 0, 3 and 6) in the main chain of p-terphenyl piperidine because of the favorable hydrophobic properties of fluorinated groups. The results show that fluorinated AEMs can enhance OH- conductivity by building more aggregated hydrophilic channels while ensuring dimensional stability. The PTF6-QAPTP AEM with more fluorinated groups has the most excellent performance at 80 °C with an OH- conductivity of 142.7 mS cm-1 and a swelling ratio (SR) of only 4.55 %. Additionally, it exhibits good alkali durability, with the OH- conductivity and quaternary ammonium (QA) cation retaining at 93.45% and 92.6%, respectively, after immersion in a 2 M NaOH solution at 80 °C for 1200 h. In addition, the power density of the PTF6-QAPTP based single cell reaches 849 mW cm-2 when the current density is 1600 mA cm-2. The PTF6-QAPTP based cell has a voltage retention of 88% after 80 h of stability testing at a constant current density of 300 mA cm-2 at 80 °C.

A novel Vestitain A from the ripe fruits of Embelia vestita Roxb.

A new compound, vestitain A (1), together with 11 known compounds were isolated from the ripe fruits of Embelia vestita Roxb., among them compounds 5,10-12 were isolated from this plant for the first time. Their structures were elucidated and characterized by detailed spectroscopic analysis. Further, the isolated new compound 1 was evaluated for its hypoglycemic effects in vivo. Our research showed that compound 1 could decrease the fasting blood glucose (FBG) by approximately 36.31% in diabetic rats at the high dose (800 mg/kg). By the Morris Water Maze experiments, we found that compound 1 had the effect of intervention on social behavior in diabetic rats, which might provide a reference basis for its development and utilization as a potential hypoglycemic drug.

Effects of the crown ether cavity on the performance of anion exchange membranes.

Anion exchange membrane fuel cells (AEMFCs) have emerged as a promising alternative to proton exchange membrane fuel cells (PEMFCs) due to their adaptability to low-cost stack components and non-noble-metals catalysts. However, the poor alkaline resistance and low OH- conductivity of anion exchange membranes (AEMs) have impeded the large-scale implementation of AEMFCs. Herein, the preparation of a new type of AEMs with crown ether macrocycles in their main chains via a one-pot superacid catalyzed reaction was reported. The study aimed to examine the influence of crown ether cavity size on the phase separation structure, ionic conductivity and alkali resistance of anion exchange membranes. Attributed to the self-assembly of crown ethers, the poly (crown ether) (PCE) AEMs with dibenzo-18-crown-6-ether (QAPCE-18-6) exhibit an obvious phase separated structure and a maximum OH- conductivity of 122.5 mS cm-1 at 80 °C (ionic exchange capacity is 1.51 meq g-1). QAPCE-18-6 shows a good alkali resistance with the OH- conductivity retention of 94.5% albeit being treated in a harsh alkali condition. Moreover, the hydrogen/oxygen single cell equipped with QAPCE-18-6 can achieve a peak power density (PPD) of 574 mW cm-2 at a current density of 1.39 A cm-2.

Stress response and tolerance mechanisms of NaHCO3 exposure based on biochemical assays and multi-omics approach in the liver of crucian carp (Carassius auratus).

The development and utilization of saline-alkaline water, an important backup resource, has received widespread attention. However, the underuse of saline-alkaline water, threatened by the single species of saline-alkaline aquaculture, seriously affects the development of the fishery economy. In this work, a 30-day NaHCO3 stress experimental study combined with analyses of untargeted metabolomics, transcriptome, and biochemical approaches was conducted on crucian carp to provide a better understanding of the saline-alkaline stress response mechanism in freshwater fish. This work revealed the relationships among the biochemical parameters, endogenous differentially expressed metabolites (DEMs), and differentially expressed genes (DEGs) in the crucian carp livers. The biochemical analysis showed that NaHCO3 exposure changed the levels of several physiological parameters associated with the liver, including antioxidant enzymes (SOD, CAT, GSH-Px), MDA, AKP, and CPS. According to the metabolomics study, 90 DEMs are involved in various metabolic pathways such as ketone synthesis and degradation metabolism, glycerophospholipid metabolism, arachidonic acid metabolism, and linoleic acid metabolism. In addition, transcriptomics data analysis showed that a total of 301 DEGs were screened between the control group and the high NaHCO3 concentration group, of which 129 up-regulated genes and 172 down-regulated genes. Overall, NaHCO3 exposure could cause lipid metabolism disorders and induce energy metabolism imbalance in the crucian carp liver. Simultaneously, crucian carp might regulate its saline-alkaline resistance mechanism by enhancing the synthesis of glycerophospholipid metabolism, ketone bodies, and degradation metabolism, at the same time increasing the vitality of antioxidant enzymes (SOD, CAT, GSH-Px) and nonspecific immune enzyme (AKP). Herein, all results will provide new insights into the molecular mechanisms underlying the stress responses and tolerance to saline-alkaline exposure in crucian carp.

Pheromones emitted by both female and male moths regulate coordination between the sexes for Agriphila aeneociliella (Lepidoptera: Crambidae).

The complex and efficient sex pheromone communication system in insects is essential for reproduction and for reproductive isolation of species. In moths, sex pheromone communication starts with male attraction to compounds emitted by females; only a few species act in the reverse. However, how the pheromones that are emitted by both sexes co-regulate and coordinate mate finding and mating remains unknown. Here, we identified both the male and female pheromones of Eastern Grass Veneer moth, Agriphila aeneociliella (Lepidoptera: Crambidae), and demonstrated their efficiency in manipulating behavioral responses of the opposite sex. Combining data from analysis of gas chromatography-electroantennogram detection, gas chromatography-mass spectrometry, and olfactory behavior assays, the female pheromone of A. aeneociliella was identified as (Z,Z,Z)-9,12,15-octadecatrienal and (Z)-9-hexadecenyl acetate, while the male pheromone was determined to be 1-nonanal. Both the 2 individual components of the female pheromone and their binary mixture were significantly attractive to males, and the 1-nonanal male pheromone induced strong electrophysiological responses in females and induced attraction of females in a Y-tube olfactory test. Depending on the concentration of 1-nonanal, its addition to the binary mixture of the female pheromone either enhanced (10-3 or 10-2  µg/µL) or reduced (1 µg/µL) the aphrodisiac effect of the mixture on males. In wind-tunnel bioassays, different concentrations of pheromones, including the binary mixture of female pheromone and the mixture of male and female pheromones, had significant effects on male behavior. Our findings suggested that the blend of both female and male pheromones plays a significant role in the sexual communication system in some moths.

Design and synthesis of fluorinated peptides for analysis of fluorous effects on the interconversion of polyproline helices.

The unique interaction between fluorine atoms has been exploited to alter protein structures and to develop synthetic and analytical applications. To expand such fluorous interaction for novel applications, polyproline peptides represent an excellent molecular nanoscaffold for controlling the presentation of perfluoroalkyl groups on their unique secondary structure. We develop approaches to synthesis fluorinated peptides to systematically investigate how the number, location and types of the fluorous groups on polyproline affect the conformation by monitoring the transition between the two major polyproline structures PPI and PPII. This work provides valuable information on how fluorous interaction affects the peptide structure and also benefits the design of functional fluorous molecules.

Prevention and control of HIV/AIDS in China: lessons from the past three decades.

ABSTRACT: In the past 37 years, human immunodeficiency virus/acquired immunodeficiency syndrome (HIV/AIDS) has undergone various major transmission routes in China, with the world most complex co-circulating HIV-1 subtypes, even the prevalence is still low. In response to the first epidemic outbreak of HIV in injecting drug users and the second one by illegal commercial blood collection, China issued the Anti-Drug Law and launched the Blood Donation Act and nationwide nucleic acid testing, which has avoided 98,232 to 211,200 estimated infections and almost ended the blood product-related infection. China has been providing free antiretroviral therapy (ART) since 2003, which covered >80% of the identified patients and achieved a viral suppression rate of 91%. To bend the curve of increasing the disease burden of HIV and finally end the epidemic, China should consider constraining HIV spread through sexual transmission, narrowing the gaps in identifying HIV cases, and the long-term effectiveness and safety of ART in the future.

Electronic nose using a bio-inspired neural network modeled on mammalian olfactory system for Chinese liquor classification.

The simplification of data processing is the frontier domain for electronic nose (e-nose) applications, whereas there are a lot of manual operations in a traditional processing procedure. To solve this problem, we propose a novel data processing method using the bio-inspired neural network modeled on the mammalian olfactory system. Through a neural coding scheme with multiple squared cosine receptive fields, continuous sensor data are simplified as the spike pattern in virtual receptor units. The biologically plausible olfactory bulb, which mimics the structure and function of main olfactory pathways, is designed to refine the olfactory information embedded in the encoded spikes. As a simplified presentation of cortical function, the bionic olfactory cortex is established to further analyze olfactory bulb's outputs and perform classification. The proposed method can automatically learn features without tedious steps such as denoising, feature extraction and reduction, which significantly simplifies the processing procedure for e-noses. To validate algorithm performance, comparison studies were performed for seven kinds of Chinese liquors using the proposed method and traditional data processing methods. The experimental results show that squared cosine receptive fields and the olfactory bulb model are crucial for improving classification performance, and the proposed method has higher classification rates than traditional methods when the sensor quantity and type are changed.

Plasma VDBP, 25(OH)D, and GSH levels predict surgical outcome in patients with cervical spondylotic myelopathy.

This study intends to investigate the predictive values of plasma Vitamin D-binding protein (VDBP), 25-hydroxyvitamin D [25(OH)D], and glutathione (GSH) levels in the outcome of cervical spondylotic myelopathy (CSM) surgery. Surgery outcomes of 236 CSM patients were determined. Recovery rate was calculated according to Japanese Orthopaedic Association (JOA) scores during follow-up. CSM patients with a recovery rate >50% were assigned with good prognosis and the rest were with fair prognosis. Preoperative and postoperative neurologic function scores were compared among groups. Plasma VDBP and 25(OH)D levels, as well as GSH levels were measured by ELISA and glutathione reductase recycling assay, respectively. Pearson's correlation coefficient was performed to analyze the correlation among plasma VDBP, 25(OH)D, and GSH levels. Receiver operating characteristic (ROC) curve was applied to evaluate the predictive value of plasma VDBP, 25(OH)D, and GSH levels for surgical outcome. Logistic regression model was used to analyze risk factors for surgical outcome. Compared with those with fair prognosis, CSM patients with good prognosis group exhibited higher postoperative neurologic function scores, plasma VDBP, 25(OH)D, and GSH levels, and better improvements in spinal cord compression and motions of the cervical vertebra. Plasma VDBP, 25(OH)D, and GSH levels were favorable prognostic factors for CSM surgical outcome. The sensitivity and specificity of plasma VDBP, plasma 25(OH)D, and plasma GSH were 89.8% and 91.7%, 85.8% and 84.4%, and 79.5% and 91.7%, respectively. Our study provides evidence that higher plasma VDBP, 25(OH)D, and GSH levels may predict better surgical outcome in CSM patients.

Controlling Ligand Spacing on Surface: Polyproline-Based Fluorous Microarray as a Tool in Spatial Specificity Analysis and Inhibitor Development for Carbohydrate-Protein Interactions.

Multivalent carbohydrate-protein interactions are essential for many biological processes. Convenient characterization for multivalent binding property of proteins will aid the development of molecules to manipulate these processes. We exploited the polyproline helix II (PPII) structure as molecular scaffolds to adjust the distances between glycan ligand attachment sites at 9, 18, and 27 Å on a peptide scaffold. Optimized fluorous groups were also introduced to the peptide scaffold for immobilization to the microarray surface through fluorous interaction to control the orientation of the helical scaffolds. Using lectin LecA and antibody 2G12 as model proteins, the binding preference to the 27 Å glycopeptide scaffold, matched the distance of 26 Å between its two galactose binding sites on LecA and 31 Å spacing between oligomannose binding sites on 2G12, respectively. We further demonstrate this microarray system can aid the development of inhibitors by transforming the selected surface-bound scaffold into multivalent ligands in solution. This strategy can be extended to analyze proteins that lacking structural information to speed up the design of potent and selective multivalent ligands.

Resistance of Wheat Accessions to the English Grain Aphid Sitobion avenae.

The English grain aphid, Sitobion avenae, is a major pest species of wheat crops; however, certain varieties may have stronger resistance to infestation than others. Here, we investigated 3 classical resistance mechanisms (antixenosis, antibiosis, and tolerance) by 14 wheat varieties/lines to S. avenae under laboratory and field conditions. Under laboratory conditions, alatae given the choice between 2 wheat varieties, strongly discriminated against certain varieties. Specifically, the 'Amigo' variety had the lowest palatability to S. avenae alatae of all varieties. 'Tm' (Triticum monococcum), 'Astron,' 'Xanthus,' 'Ww2730,' and 'Batis' varieties also had lower palatability than other varieties. Thus, these accessions may use antibiosis as the resistant mechanism. In contrast, under field conditions, there were no significant differences in the number of alatae detected on the 14 wheat varieties. One synthetic line (98-10-30, a cross between of Triticum aestivum (var. Chris) and Triticum turgidum (var. durum) hybridization) had low aphid numbers but high yield loss, indicating that it has high antibiosis, but poor tolerance. In comparison, 'Amigo,' 'Xiaoyan22,' and some '186Tm' samples had high aphid numbers but low yield loss rates, indicating they have low antibiosis, but good tolerance. Aphid population size and wheat yield loss rates greatly varied in different fields and years for '98-10-35,' 'Xiaoyan22,' 'Tp,' 'Tam200,' 'PI high,' and other '186Tm' samples, which were hybrid offspring of T. aestivum and wheat related species. Thus, these germplasm should be considered for use in future studies. Overall, S. avenae is best adapted to 'Xinong1376,' because it was the most palatable variety, with the greatest yield loss rates of all 14 wheat varieties. However, individual varieties/lines influenced aphid populations differently in different years. Therefore, we strongly recommend a combination of laboratory and long-term field experiments in targeted planting regions to identify varieties/lines that consistently show high resistance to S. avenae infestation.

Impact of aphid alarm pheromone release on virus transmission efficiency: When pest control strategy could induce higher virus dispersion.

Aphids cause serious damages to crops not only by tacking sap but also by transmitting numerous viruses. To develop biological control, the aphid alarm pheromone, namely E-ß-farnesene (EßF), has been demonstrated to be efficient to repel aphids and as attract beneficials, making it a potential tool to control aphid pests. Considering aphids also as virus vectors, changes of their behavior could also interfere with the virus acquisition and transmission process. Here, a combination of two aphid species and two potato virus models were selected to test the influence of EßF release on aphid and virus dispersion under laboratory conditions. EßF release was found to significantly decrease the population of Myzus persicae and Macrosiphum euphorbiae around the infochemical releaser but simultaneously also increasing the dispersal of Potato Virus Y (PVY). At the opposite, no significant difference for Potato Leaf Roll Virus (PLRV) transmission efficiency was observed with similar aphid alarm pheromone releases for none of the aphid species. These results provide some support to carefully consider infochemical releasers not only for push-pull strategy and pest control but also to include viral disease in a the plant protection to aphids as they are also efficient virus vectors. Impact of aphid kinds and transmission mechanisms will be discussed according to the large variation found between persistent and non persistent potato viruses and interactions with aphids and related infochemicals.

Anti-phytopathogenic activity of sporothriolide, a metabolite from endophyte Nodulisporium sp. A21 in Ginkgo biloba.

Phytopathogenic fungi such as Rhizoctonia solani and Sclerotinia sclerotiorum caused multiple plant diseases resulting in severe loss of crop production. Increasing documents endorsed that endophytes are a striking resource pool for numerous metabolites with various bioactivities such as anti-fungal. Here we reported the characterization and anti-phytopathogenic activity of sporothriolide, a metabolite produced by Nodulisporium sp. A21-an endophytic fungus in the leaves of Ginkgo biloba. Among the total twenty-five endophytic fungi isolated from the healthy leaves of G. biloba, the fermentation broth (FB) of the strain A21 was found potently inhibitory activity against R. solani and S. sclerotiorum using mycelia growth inhibition method. A21 was then identified as Nodulisporium sp., the asexual stage of Hypoxylon sp., by microscopic examination and ITS rDNA sequence data comparison. Under the bioassay-guided fractionation, sporothriolide was isolated from the petroleum ether extract of the FB of A21, whose structure was established by integrated interpretation of HR-ESI-MS and (1)H- and (13)C-NMR. Furthermore, the crystal structure of sporothriolide was first reported. In addition, sporothriolide was validated to be potently antifungal against R. solani, S. sclerotiorum and inhibit conidium germination of Magnaporthe oryzae in vitro and in vivo, indicating that it could be used as a lead compound for new fungicide development.

[Ecological functions of E-ß-farnesene on aphids and their natural enemies in potato field.] / 反-ß-æ³•å°¼çƒ¯å¯¹é©¬é“ƒè–¯èšœè™«åŠå ¶å¤©æ•Œçš„ç”Ÿæ€æ•ˆåº”.

As a most common component of aphid alarm pheromone, E-ß-farnesene (EßF) could not only dispel aphids, but also modify some behavioral responses of their natural enemies. In order to investigate the ecological function of EßF, its influence on the population dynamics of Myzus persicae (Sulzer), Aphis gossypii (Glover), Macrosiphum euphorbiaein (Thomas) and their natural enemies was studied in potato fields. The results showed that there were significantly lower aphid abundance (2012, 2013), higher ladybird beetle abundance (2012, 2013), and higher mummified aphid abundance (2012) on potato plants in EßF treated plots (100 µL per week). The numbers of aphids at the distances of 1 m and 5 m from EßF releaser were significantly lower compared to 10 m in 2012, and the aphid number was significantly lower at the distance of 1 m compared to 5 m and 10 m in 2013. Moreover, significantly higher parasitoid and hoverfly numbers in 2012 and higher numbers of ladybird beetles in 2013 were observed in yellow traps in EßF treated plots. The results suggested that EßF could suppress aphid population growth within a certain distance in potato fields.

New flavonoid from Patrinia villosa.

CONTEXT: Patrinia villosa (Thunb.) Juss (Valerianaceae) is an important ancient herbal medicine widely used for inflammation, wound healing, and abdominal pain. But little is known of the phytochemical constituents of this herbal plant. OBJECTIVE: The objective of this study is to isolate and identify the bioactive components from P. villosa. MATERIALS AND METHODS: A 70% EtOH extract of P. villosa was subjected to normal-phase silica, ODS silica gel column chromatography, and semi-preparative HPLC chromatography after partitioned successively with light petroleum, dichloromethane and n-BuOH. Chemical structures of the compounds were elucidated by spectroscopic methods including UV, 1D-NMR, 2D-NMR, HR-ESI-MS, and CD spectra. The cytotoxic activity of the new component was determined with the SMMC-7721 cell line using the MTT method after incubation for 48 h. RESULTS: A new flavonoid named patriniaflavanone A (1) along with four known compounds was isolated from P. villosa. The four known compounds were identified as luteolin 7-O-glucuronide-6″-methyl ester (2), p-hydroxyphenylacetic acid methyl ester (3), trans-caffeic acid (4), and trans-caffeic acid methylate (5) by comparison of their spectral data with the reported data. The IC50 value of patriniaflavanone A (1) on SMMC-7721 was 61.27 µM. DISCUSSION AND CONCLUSION: This is the first report on the isolation and identification of patriniaflavanone A (1), and compounds 2-5 were isolated for the first time from the title plant. Patriniaflavanone A (1) exhibited moderate cytotoxic activity.

[Inhibitory Effect of the Excretory/Scretory Proteins of Trichinella spiralis on Proliferation of Human Hepatocellular Carcinoma HepG2 Cell line].

Human hepatocellular carcinoma HepG2 Cell line were cultured with different concentrations of excretory/secretory proteins from Trichinella spiralis, and MTT assay was used to evaluate the cell inhibition rate. After co-cultured with 300 µg/ml excretory/secretory proteins for 24 h, the HepG2 cells were observed under a fluorescence microscope with AO and EB staining. When co-cultured with 75 µg/ml excretory/secretory proteins for 24 h, the HepG2 cells were quantified by flow cytometry using Annexin V-FITC/PI stain, and the expression of cleaved-caspase 9 was detected by immunofluorescence assay. The proliferation of HepG2 cells was inhibited significantly by excretory/secretory proteins in a dosage dependant manner. Under fluorescence microscope, some HepG2 cells presented typical apoptotic morphologic changes and the cleaved-caspase 9 protein expression was higher than that of the control. The early and late apoptotic cells and necrotic ones occupied 17.9%, 7.3%, and 6.6%, respectively.

Metastatic lung adenocarcinoma to the bladder: A case report.

Urothelial cancer is the most frequently diagnosed type of malignant tumor in the bladder, of which primary adenocarcinoma accounts for a small percentage. Secondary malignancies, in particular metastatic adenocarcinoma from the lung, are exceedingly rare, with only six cases previously reported in the literature. The present study describes the case of a 71-year-old Chinese male patient with known lung cancer for >2 years, who was diagnosed with metastatic adenocarcinoma to the bladder. The histopathological characteristics and immunohistochemical features of the patient are reported. It was proposed that pathologists should consider the possibility of metastatic adenocarcinoma from the lung, rather than assume a diagnosis of primary adenocarcinoma of the bladder or direct invasion of adenocarcinoma from the surrounding organs. Furthermore, it is essential to determine the medical history of each patient and observe the immunohistochemical features of all tumors prior to diagnosis.

[Synthesis and antitumor activity of fluoroquinolon-3-yl-s-triazole sulfide ketones and their derivatives from ciprofloxacin].

To discover an efficient strategy for the conversion of the antibacterial activity of fluoroquinolones into the antitumor activity, the three series of C-3 s-triazole-based derivatives including sulfide ketones (6a-6g), thiosemicarbazones (7a-7g) and fused heterocyclic thiazolotriazoles (8a-8g) were synthesized from ciprofloxacin (1), respectively. The structures were characterized by elemental analysis and spectral data. The antitumor activity was tested against three tumor cell lines (Hep-3B, Capan-1 and HL60) using the MTT assay. The three types of compounds all exhibited stronger anti-proliferative activities than ciprofloxacin in the test. The order of their activities was in compounds 7>8>6, and the order of selectivity against cancer cell lines was Capan-1, Hep-3B and HL60. Meanwhile, the SAR revealed that some compounds with electron-drawing group substituted such as fluoro- and nitro-phenyl compounds (6f, 7f, 8f) and (6g, 7g, 8g) displayed more significant activity than the control compounds, especially the IC50 values of thiosemicarbazone compounds 7f and 7g against Capan-1 was comparable to doxorubicin. Thus, a five-membered triazole as the C-3 bioisostere modified with the functionalized side-chain of sulfide-ketone thiosemicarbazone warrants special attention and further investigation.